Publications by authors named "Christian Brudy"
Article Synopsis
- Macrocycles are seen as effective tools for targeting hard-to-reach proteins inside cells, but improving them from initial linear structures is still a work in progress.
- Researchers studied linker modification to enhance macrocycle properties, focusing on FKBP51 and producing over 140 versions with different linkers.
- They discovered that these modifications led to better affinity, stability, and solubility of the macrocycles compared to earlier models, and emphasized the importance of understanding the 3D shapes of these molecules in drug development.
Article Synopsis
- Macrocycles are natural and synthetic compounds that can enhance the ability of bioactive molecules to penetrate cells, with emerging guidelines for their design.
- Even medium-sized macrocycles exhibit significant flexibility in shape, even while attached to target proteins, which allows for diverse conformations.
- Minor linker modifications in these macrocycles can lead to new ligand formations with improved binding properties for important therapeutic targets, highlighting the unique benefits of macrocyclic structures in drug development.
Macrocycles are one of nature's preferred choices to generate large but cell-permeable bioactive molecules. Macrocyclization is increasingly prominent in medicinal chemistry beyond natural products, especially for difficult-to-drug targets. However, strategies to best exploit the potential of macrocycles are only beginning to emerge.
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